甲基普賴鬆 / 甲基培尼皮質醇
Methylprednisolone
6alpha-methylprednisolone
別名: Depo-Medrol · Solu-Medrol · A-Methapred · Depo-Medrone · Solu-Medrone · 6alpha-methylprednisolone · methylprednisolonum · NSC-19987 · Methylprednisolone acetate · Methylprednisolone sodium succinate
由 VetSheet 獸醫團隊審訂更新於 2026年4月5日本內容以實證獸醫文獻為本
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Labeled uses (Oral) | Dogs weighing 5-15 lbs: 2 mg; Dogs weighing 15-40 lbs: 2-4 mg; Dogs weighing 40-80 lbs: 4-8 mg; these total daily doses should be divided | PO | q6-10h | — | 🌎 NA |
| Labeled uses (Injectable) | 2-120 mg (average 20 mg) | IM | May repeat at weekly intervals | — | 🌎 NA |
| Intralesional (sub-lesional) use | 10-40 mg total dose | intralesional | — | — | 🌎 NA |
- Labeled uses (Oral): Divide total daily dose and give 6-10 hours apart.
- Labeled uses (Injectable): Depending on breed (size), severity of condition, and response.
- Intralesional (sub-lesional) use: A sufficient volume of 20 mg/mL methylprednisolone acetate is used to undermine the lesion.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Labeled uses (Oral) | Cats weighing 5-15 lbs: 2 mg; Cats weighing >15 lbs: 2-4 mg; these total daily doses should be divided | PO | q6-10h | — | 🌎 NA |
| Labeled uses (Injectable) | up to 20 mg (average 10 mg) | IM | May repeat at weekly intervals | — | 🌎 NA |
| Intralesional (sub-lesional) use | 10-40 mg total dose | intralesional | — | — | 🌎 NA |
- Labeled uses (Oral): Divide total daily dose and give 6-10 hours apart.
- Labeled uses (Injectable): Depending on breed (size), severity of condition, and response.
- Intralesional (sub-lesional) use: A sufficient volume of 20 mg/mL methylprednisolone acetate is used to undermine the lesion.
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Antiinflammatory (glucocorticoid effects) | 200 mg | IM | repeated as necessary | — | 🌎 NA |
| Intra-articular use | 100 mg | IA | — | — | 🌎 NA |
- Antiinflammatory (glucocorticoid effects): Labeled use.
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
概覽
甲基普賴鬆是一種合成的中效糖皮質激素，其效力約為氫化可的松的4至5倍，且幾乎不具鹽皮質激素活性。在獸醫學中廣泛用於其強效的抗發炎和免疫抑制特性。
臨床要點與劑型：
- 甲基普賴鬆鹼基： 用於口服錠劑，適合維持或遞減療法。
- 醋酸甲基普賴鬆 (Depo-Medrol®)： 微晶懸浮液，用於肌肉內、病灶內或關節內注射。吸收緩慢，提供長效儲積作用（數週至數月）。注意： 可能導致嚴重且長期的下視丘-腦下垂體-腎上腺 (HPA) 軸抑制。
- 琥珀酸鈉甲基普賴鬆 (Solu-Medrol®)： 高度水溶性酯類，專為急性危急情況（如脊髓創傷、嚴重過敏反應、休克）的快速靜脈注射而設計，儘管高劑量用於休克/創傷的爭議日益增加。
雖然非常有效，但糖皮質激素治療的目標始終是在最短時間內使用最低有效劑量，以盡量減少全身性不良反應，特別是醫源性腎上腺皮質機能亢進（庫興氏症候群）。
作用機制
Glucocorticoids exert their effects by diffusing across cell membranes and binding to specific cytoplasmic glucocorticoid receptors (GR).
- Genomic Pathway: The receptor-ligand complex translocates to the nucleus → binds to glucocorticoid response elements (GREs) on target genes → alters gene transcription.
- Anti-inflammatory Mechanism: They induce the synthesis of lipocortin-1 (annexin-1) → inhibits phospholipase A2 → blocks the release of arachidonic acid from membrane phospholipids → profoundly decreases the synthesis of pro-inflammatory prostaglandins and leukotrienes.
- Immunosuppressive Mechanism: They suppress the transcription of inflammatory cytokines (e.g., IL-1, IL-2, IL-6, TNF-alpha), inhibit macrophage and neutrophil migration/function, and induce apoptosis in lymphocytes.
- Metabolic Effects: Stimulate hepatic gluconeogenesis, promote protein catabolism, and redistribute lipid stores.
安全性與警告
禁忌症
- Systemic fungal infections (unless used for Addison's replacement)
- Viral infections
- Arrested tuberculosis
- Peptic or corneal ulcers
- Acute psychoses
- Cushingoid syndrome
- Idiopathic thrombocytopenia (for IM administration)
- Acute local infections (for intrasynovial/intratendinous use)
- Chronic systemic therapy using sustained-release injectable forms
- Pregnant animals
- Renal disease
- Diabetes mellitus
不良反應
- Polyuria (PU), polydipsia (PD), polyphagia (PP)
- Iatrogenic hyperadrenocorticism (Cushingoid signs) with sustained use
- Weight gain and lipidemias
- Dull, dry haircoat and alopecia
- Muscle wasting and weakness
- Gastrointestinal ulceration, vomiting, diarrhea, melena, hematochezia
- Elevated liver enzymes (ALP, ALT) and hepatopathy
- Pancreatitis
- Activation or worsening of diabetes mellitus (especially in cats)
- Behavioral changes (depression, lethargy, viciousness, panting)
- Extracellular hyperglycemia leading to volume expansion and potential CHF (cats)
- Hypothalamic-pituitary-adrenal (HPA) axis suppression
- Adrenal atrophy
- Weight loss (catabolic effect)
- Cutaneous atrophy (thinning of skin)
- Iatrogenic hyperadrenocorticism (Cushing's syndrome)
- Diarrhoea
- Increased urine glucose levels
- Decreased serum T3 and T4 levels
- Impaired wound healing
- Delayed recovery from infections
注意事項
Tapering Required: Animals receiving systemic glucocorticoids (other than short 'burst' therapy) must be tapered off slowly to allow endogenous ACTH and corticosteroid function to recover. Abrupt withdrawal can precipitate an Addisonian crisis.
- Stress Dosing: Additional glucocorticoids may be needed during stressors (surgery, trauma, illness) during the tapering process.
- Use with Caution: In patients with diabetes mellitus, osteoporosis, predisposition to thrombophlebitis, hypertension, congestive heart failure (CHF), and renal insufficiency.
- Pregnancy: FDA Category C. May cause teratogenic effects in early pregnancy. Exogenous steroids can induce parturition in the latter stages of pregnancy in horses and ruminants.
- Nursing Dams: Glucocorticoids enter milk and may inhibit growth or interfere with endogenous corticosteroid production in nursing offspring.
藥物相互作用
May cause hypokalemia; potential for CHF and cardiac enlargement
Combination in epidurals has caused serious CNS injuries and death
May lead to profound muscle weakness in myasthenia gravis patients
Glucocorticoids may reduce salicylate blood levels
May increase the metabolism of glucocorticoids and decrease blood levels
Glucocorticoids may inhibit hepatic metabolism of cyclophosphamide
May mutually inhibit hepatic metabolism, increasing blood levels of both drugs
May cause hypokalemia
May reduce methylprednisolone blood levels
May potentiate the effects of methylprednisolone
Insulin requirements may increase due to glucocorticoid-induced insulin resistance
May decrease metabolism of glucocorticoids; ketoconazole may induce adrenal insufficiency upon withdrawal
May decrease metabolism of glucocorticoids and increase blood levels
May alter steroid metabolism; higher steroid doses may be needed
Increased risk of severe gastrointestinal ulceration
May increase metabolism of glucocorticoids and decrease blood levels
May increase metabolism of glucocorticoids and decrease blood levels
Virus replication may be augmented; diminished immune response to vaccines
May affect INR values; requires monitoring
Increased risk of hypokalaemia
Enhanced metabolism of corticosteroids, potentially reducing their efficacy
Decreased metabolism of corticosteroids, potentially increasing their effects and toxicity
監測
- Weight, appetite, and signs of edema
- Serum and/or urine electrolytes
- Total plasma proteins, albumin
- Growth and development in young animals
- ACTH stimulation test (if iatrogenic Cushing's or Addison's is suspected)
- Clinical signs of iatrogenic hyperadrenocorticism (PU/PD, polyphagia, weight gain)
- Blood glucose levels (especially in diabetic or pre-diabetic patients)
- Serum electrolytes (specifically potassium)
- Thyroid panel (T3 and T4 may be artificially decreased)
- Signs of gastrointestinal ulceration (melena, vomiting blood)
藥物動力學
半衰期
吸收
Orally administered methylprednisolone is relatively well absorbed. The acetate IM injection is slowly absorbed and can have a duration of effect of weeks to months. The sodium succinate IV injection is water soluble and very fast acting.
分佈
Extensively distributed throughout the body.
代謝
The liver is the primary site for metabolism (oxidation).
排除
Most of the drug is excreted renally as metabolites.
過量
Short-term administration of massive doses is unlikely to cause harmful effects, though one case of acute CNS effects in a dog after accidental ingestion has been reported. If acute overdose occurs, provide supportive treatment as required.
Chronic Overdosage: Chronic usage leads to serious adverse effects, primarily iatrogenic hyperadrenocorticism (Cushing's syndrome), characterized by profound metabolic, dermatologic, and immunosuppressive changes.
可用產品
劑型
- Injectable suspension (Acetate)
- Powder for injection (Sodium Succinate)
- Injectable depot suspension: 40 mg/ml
- Injectable powder for reconstitution: 125 mg, 500 mg
- Oral tablets: 2 mg, 4 mg
獸醫用
- Methylprednisolone Tablets: 4 mg (Medrol®)
- Methylprednisolone Acetate Injection: 20 mg/mL, 40 mg/mL (Depo-Medrol®)
- Depo-Medrone 40 mg/ml depot suspension
- Solu-Medrone 125 mg powder for reconstitution
- Solu-Medrone 500 mg powder for reconstitution
- Medrone 2 mg tablets
- Medrone 4 mg tablets
人用標示
- Methylprednisolone Oral Tablets: 2 mg, 4 mg, 8 mg, 16 mg, 24 mg, 32 mg (Medrol®)
- Methylprednisolone Acetate Injection: 20 mg/mL, 40 mg/mL, 80 mg/mL (Depo-Medrol®)
- Methylprednisolone Sodium Succinate Powder for Injection: 40 mg, 125 mg, 500 mg, 1 gram, 2 grams per vial (Solu-Medrol®, A-Methapred®)
各地核准狀態
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store commercially available products at room temperature (15-30°C). Avoid freezing the acetate injection. After reconstituting the sodium succinate injection, store at room temperature and use within 48 hours; only use solutions that are clear.
飼主須知
寵物主人重要指引：
- 切勿突然停藥： 未經獸醫師同意，絕對不要突然停止使用此藥物。使用此藥期間，身體自然的類固醇分泌會暫停，突然停藥可能導致危及生命的危機。您的獸醫師會提供逐漸減量的計畫。
- 預期的副作用： 寵物在服藥期間喝水量增加、排尿頻繁和食慾大增是非常常見的現象。請確保牠們隨時有乾淨的飲水，並增加帶牠們上廁所的次數。
- 注意嚴重症狀： 如果您發現嚴重的副作用，如嘔吐、排出黑色/柏油狀糞便、血便極度嗜睡、異常喘氣或行為發生重大改變，請立即聯繫您的獸醫師。
- 遵照指示： 請完全依照處方給藥。如果採用隔日給藥的計畫，在日曆上做記號有助於避免漏藥。
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